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PDA 2 > 2.6 > Flashcards

2.6 Flashcards

(52 cards)

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1
Q

Reactions that increase polarity?

A

Phase 1

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2
Q

What type of functional groups do Phase 1 add?

A

Polar

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3
Q

Which phase generally terminates biological activity?

A

Phase 1

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4
Q

Oxidation, Reduction, Hydrolysis

A

Phase 1 reactions

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5
Q

Most frequently occuring type of Phase 1 reaction?

A

Oxidation

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6
Q

A subcellular fraction

A

Microsomes

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7
Q

Microsomes contain?

A

fragments of the endoplasmic reticulum

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8
Q

A multicomponent electron transport system?

A

Cytochorome P450

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9
Q

Cyt 450

A

Serves as substrate binding site and Oxygen binding site

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10
Q

NADPH Cytochrome P 450 Reductase

A

Contains FAD and FMN. Shuttles electrons from NADPH to P450

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11
Q

Where do different isoforms of Cyt P450 exist?

A

liver

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12
Q

Each Cyt P450 has a different?

A

substrate selectivity

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13
Q

What are MFO’s made up of?

A

A family of heme proteins known as Cytochromes P450

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14
Q

Hydroxylation

A

Microsomes

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15
Q

Dealkylation

A

Microsomes

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16
Q

Oxide formation

A

Microsomes

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17
Q

Desulfurization

A

Microsomes

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18
Q

Dehalogenation

A

Microsomes

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19
Q

Alcohol oxidation

A

Soluble and Microsomes

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20
Q

Aldehyde oxidation

A

soluble

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21
Q

Deamination

Study These Flashcards
A

Microsomes and Mitochondria

22
Q

Reductive Reactions

Study These Flashcards
A
  1. May be reversible when coupled with oxidative reactions
  2. Usually occur at groups with multiple bonds
  3. Usually seen when one or both atoms are heteroatoms
23
Q

Aldehyde reduction

24
Q

Azoreduction

25
Nitroreduction
microsomes, soluble
26
What do phase II reactions do?
increase solubility, by bringing things together
27
What type of groups does a Phase II attach?
small, polar, ionizable endogenous compounds such as glucuronic acid, glycine, and sulfate
28
Where does Phase II reactions attach the conjugating groups?
To polar functional group generated in Phase I
29
What type of reaction is Glutathione (GSH)
Phase II
30
What does a Glutathione conjugation do?
protects the body from toxic, electrophilic compounds and metabolic activation products.
31
Type of molecule is GSH?
nucleophilie
32
What phase increases the H2O solubility more?
Phase II
33
What 2 reactions decrease the H2O solubility?
Methylation and acetylation
34
What is the most important organ in drug metabolism?
The liver
35
Drugs taken orally travel to the liver via the?
Portal vein system after absorption
36
First past effect.
Following absorption from the gi tract drugs travel directly to the liver, where some are extensively metabolized before reaching the systemic circulation.
37
Which drug is not an effective on oral administration because of the first pass effect?
Lidocaine
38
Extrahepatic metabolism
Anywhere besides the liver
39
What is in the intestinal wall that hydroyzes glucuronide conjugates found in the bile and release free drug?
Beta-glucuronidases
40
Enterohepatic recirculation
reabsorption of free drug back across the gut wall into the systemic circulation
41
What enzymes are contained in the lumen?
Azoreductases Nitroreductases Sulfatases
42
Mammal that doesnt acetylate?
Dogs
43
Mammal that makes sulfates, but not glucuronides?
Cats
44
Mammal that makes glucuronides, but not sulfates?
Pig
45
Mammal that acetylates, makes glucuronidate and sulfate?
Humans
46
What ethnic groups are rapid acetylators of isoniazid?
Eskimos and Asians
47
5 factors influencing metabolism
1. Genetic Factors 2. Sex 3. Physiological Differences 4. Pharmacodynamic factors 5. Environmental factors
48
Example of pharmacodynamic factors?
Dose of drug. The concentration could saturate all the enzymes.
49
Enzyme Inhibitors
Poisoning of enzymes by toxic chemicals such as carbon monoxide, or pesticides may alter metabolism
50
Enzyme Inducers
Prolonged treatment with phenobarbital or phenytoin will increase the concentration of microsomal enzymes and thus, decrease the half-life of many drugs.
51
Examples of enzyme inducers
Phenobarbital Benzopyrene 3-methylcholanthrine
52
Largest CYP 450 Isoform
2A4/5

PDA 2 (6 decks)

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